title: Samarium-153 and lutetium-177 chelation properties of selected macrocyclic and acyclic ligands.
abstract: We describe a simple in vitro characterization of chelation that is useful when choosing an appropriate ligand-metal combination for clinical applications. These properties include the effect of concentration on chelation efficiency, time to maximum chelation, and stability in acidic and serum environments. The macrocyclic ligands nitro-DOTA and nitro-PADOTA, the acyclic ligands nitro-CHX-A-DTPA, nitro-MX-DTPA, DTPA, and a novel terpyridine ligand, TMT-amine, were evaluated as chelate complexes of both intermediate energy beta-emitting lanthanides lutetium-177 and samarium-153. The data were compared to results obtained in a previously published study with yttrium-90. Acid lability, time to achieve maximum chelation, and stability in human serum are properties unique to each ligand-metal combination and should be evaluated prior to choosing an appropriate combination for therapeutic applications. Concentration dependence and duration of chelation are general properties of lanthanide and yttrium chelation that can be applied to an appropriate ligand-metal combination to achieve optimum chelation efficiencies.
authors.affiliation: Department of Molecular Sciences, Glaxo Wellcome, Inc., Research Triangle Park, NC 27709, USA.
authors.forename: J B
authors.initials: JB
authors.lastname: Stimmel
authors.forename: F C
authors.initials: FC
authors.lastname: Kull
mesh_terms: D002614:Chelating Agents / Q000737:chemistry*; D002855:Chromatography, Thin Layer; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007202:Indicators and Reagents; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D008187:Lutetium / Q000097:blood / Q000737:chemistry*; D011868:Radioisotopes; D012493:Samarium / Q000097:blood / Q000737:chemistry*
chemical_list: D002614:Chelating Agents; D007202:Indicators and Reagents; D008024:Ligands; D011868:Radioisotopes; D012493:Samarium; D008187:Lutetium